Writers and readers of histone acetylation: structure, mechanism, and inhibition
R Marmorstein, MM Zhou - Cold Spring Harbor …, 2014 - cshperspectives.cshlp.org
Histone acetylation marks are written by histone acetyltransferases (HATs) and read by
bromodomains (BrDs), and less commonly by other protein modules. These proteins …
bromodomains (BrDs), and less commonly by other protein modules. These proteins …
Bromodomains as therapeutic targets
Acetylation of lysine residues is a post-translational modification with broad relevance to
cellular signalling and disease biology. Enzymes that 'write'(histone acetyltransferases …
cellular signalling and disease biology. Enzymes that 'write'(histone acetyltransferases …
Prostate cancer–associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4
The bromodomain and extraterminal (BET) family of proteins comprises four members—
BRD2, BRD3, BRD4 and the testis-specific isoform BRDT—that largely function as …
BRD2, BRD3, BRD4 and the testis-specific isoform BRDT—that largely function as …
BRD4-directed super-enhancer organization of transcription repression programs links to chemotherapeutic efficacy in breast cancer
B Liu, X Liu, L Han, X Chen, X Wu… - Proceedings of the …, 2022 - National Acad Sciences
BRD4 is well known for its role in super-enhancer organization and transcription activation
of several prominent oncogenes including c-MYC and BCL2. As such, BRD4 inhibitors are …
of several prominent oncogenes including c-MYC and BCL2. As such, BRD4 inhibitors are …
Most random gene expression signatures are significantly associated with breast cancer outcome
D Venet, JE Dumont, V Detours - PLoS computational biology, 2011 - journals.plos.org
Bridging the gap between animal or in vitro models and human disease is essential in
medical research. Researchers often suggest that a biological mechanism is relevant to …
medical research. Researchers often suggest that a biological mechanism is relevant to …
The Brd4 extraterminal domain confers transcription activation independent of pTEFb by recruiting multiple proteins, including NSD3
S Rahman, ME Sowa, M Ottinger, JA Smith… - … and cellular biology, 2011 - Taylor & Francis
Bromodomain protein 4 (Brd4) plays critical roles in development, cancer progression, and
virus-host pathogenesis. To gain mechanistic insight into the various biological functions of …
virus-host pathogenesis. To gain mechanistic insight into the various biological functions of …
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Small molecule inhibitor of the bromodomain and extraterminal domain (BET) family
proteins is a promising option for cancer treatment. However, current BET inhibitors are …
proteins is a promising option for cancer treatment. However, current BET inhibitors are …
BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain
BN Devaiah, BA Lewis, N Cherman… - Proceedings of the …, 2012 - National Acad Sciences
The bromodomain protein, BRD4, has been identified recently as a therapeutic target in
acute myeloid leukemia, multiple myeloma, Burkitt's lymphoma, NUT midline carcinoma …
acute myeloid leukemia, multiple myeloma, Burkitt's lymphoma, NUT midline carcinoma …
[HTML][HTML] Differentiation-state plasticity is a targetable resistance mechanism in basal-like breast cancer
Intratumoral heterogeneity in cancers arises from genomic instability and epigenomic
plasticity and is associated with resistance to cytotoxic and targeted therapies. We show …
plasticity and is associated with resistance to cytotoxic and targeted therapies. We show …
[HTML][HTML] Opposing functions of BRD4 isoforms in breast cancer
Summary Bromodomain-containing protein 4 (BRD4) is a cancer therapeutic target in
ongoing clinical trials disrupting primarily BRD4-regulated transcription programs. The role …
ongoing clinical trials disrupting primarily BRD4-regulated transcription programs. The role …